发明名称 |
INDOLI ZINE DERIVATIVES AND THEIR USE AS CRTH2 ANTAGONISTS |
摘要 |
Compounds of formula (I) are ligands of the CRTH2 receptor and are useful in the treatment of respiratory disease: Formula (I) wherein R<SUB>1</SUB>, R<SUB>2</SUB>, R<SUB>3</SUB> and R<SUB>4</SUB> each independently are hydrogen, C<SUB>1</SUB>C<SUB>6</SUB>alkyl, fully or partially fluorinated C<SUB>1</SUB>C<SUB>6</SUB>alkyl, halo, -S(O)<SUB>n</SUB>R<SUB>10</SUB>, -SO<SUB>2</SUB>N(R<SUB>10</SUB>)<SUB>2</SUB>, -N(R<SUB>10</SUB>)<SUB>2</SUB>, -C(O)N(R<SUB>10</SUB>)<SUB>2</SUB>, -NR<SUB>10</SUB>C(O)R<SUB>9</SUB>, -CO<SUB>2</SUB>R<SUB>10</SUB>, -C(O)R<SUB>9</SUB>, -NO<SUB>2</SUB>, -CN or -OR<SUB>11</SUB>; wherein each R<SUB>9</SUB> is independently C<SUB>1</SUB>C<SUB>6</SUB>alkyl, aryl, heteroaryl; R<SUB>10</SUB> is independently hydrogen, C<SUB>1</SUB>C<SUB>6</SUB>alkyl, aryl, or heteroaryl; R<SUB>11</SUB> is hydrogen, C<SUB>1</SUB>C<SUB>6</SUB>alkyl, fully or partially fluorinated C<SUB>1</SUB>C<SUB>6</SUB>alkyl or a group -SO<SUB>2</SUB>R<SUB>9</SUB>; n is 0, 1 or 2; R5 is C<SUB>1</SUB>C<SUB>6</SUB>alkyl, fully or partially fluorinated C<SUB>1</SUB>C<SUB>6</SUB>alkyl , C<SUB>1</SUB>C<SUB>6</SUB>alkenyl , C<SUB>1</SUB>C<SUB>6</SUB>alkynyl, optionally substituted aryl, or optionally substituted heteroaryl; R<SUB>6</SUB> is hydrogen, C<SUB>1</SUB>C<SUB>6</SUB>alkyl or fully or partially fluorinated C<SUB>1</SUB>C<SUB>6</SUB>alkyl ; R<SUB>7</SUB> and R<SUB>8</SUB> are independently hydrogen or C<SUB>1</SUB>C<SUB>6</SUB>alkyl, or R<SUB>7</SUB> and R<SUB>8</SUB> together with the atom to which they are attached form a cycloalkyl group; and X is -CHR<SUB>6</SUB>-, -S(O)<SUB>n</SUB>-, -NR<SUB>6</SUB>SO<SUB>2</SUB>- or -SO<SUB>2</SUB>NR<SUB>6</SUB>- wherein n is 0, 1 or 2. |
申请公布号 |
WO2006136859(A3) |
申请公布日期 |
2007.04.05 |
申请号 |
WO2006GB02341 |
申请日期 |
2006.06.26 |
申请人 |
ARGENTA DISCOVERY LTD.;HYND, GEORGE;RAY, NICHOLAS, CHARLES;FINCH, HARRY;MIDDLEMISS, DAVID;CRAMP, MICHAEL, COLIN;BLANEY, PAUL, MATTHEW;WILLIAMS, KAREN;GRIFFON, YAN;HARRISON, TREVOR, KEITH;CRACKETT, PETER |
发明人 |
HYND, GEORGE;RAY, NICHOLAS, CHARLES;FINCH, HARRY;MIDDLEMISS, DAVID;CRAMP, MICHAEL, COLIN;BLANEY, PAUL, MATTHEW;WILLIAMS, KAREN;GRIFFON, YAN;HARRISON, TREVOR, KEITH;CRACKETT, PETER |
分类号 |
C07D471/04;A61K31/437;A61P11/06;A61P11/08;A61P17/00;A61P19/02;A61P29/00;A61P37/08 |
主分类号 |
C07D471/04 |
代理机构 |
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地址 |
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